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| United States Patent |
5,776,438
|
|
Tokue
, et al.
|
July 7, 1998
|
External preparation
Abstract
An external preparation containing DL-.alpha.-tocopherol 2- L-ascorbic
phosphoric diester and/or a salt thereof, and at least one ultraviolet
absorbing agent. The cross-linking of collagen is suppressed and an
excellent cutaneous aging resisting effect is obtained.
| Inventors:
|
Tokue; Wataru (Yokohama, JP);
Ito; Kenzo (Yokohama, JP);
Tominaga; Naoki (Tokyo, JP)
|
| Assignee:
|
Shiseido Co., Ltd. (Tokyo, JP)
|
| Appl. No.:
|
645681 |
| Filed:
|
May 14, 1996 |
| Current U.S. Class: |
424/59; 424/70.9; 424/401; 514/148; 514/454 |
| Intern'l Class: |
A61K 007/42; A61K 031/66 |
| Field of Search: |
424/401,59,70.9
574/454,148
|
References Cited
U.S. Patent Documents
| 4564686 | Jan., 1986 | Ogata | 549/220.
|
| 5053222 | Oct., 1991 | Takasu et al. | 424/7.
|
Primary Examiner: Dean; Karen A.
Attorney, Agent or Firm: Townsend&Banta
Parent Case Text
CROSS REFERENCE TO A RELATED APPLICATIONS
This is a Continuation-In-Part patent application of application Ser. No.
08/371,484 filed Jan. 11, 1995, now abandoned, which is a file wrapper
continuation application of application Ser. No. 07/854,624 filed Jun. 26,
1992 which claims priority of PCT application No. PCT/JP90/01383 filed
Oct. 18, 1990.
Claims
What is claimed is:
1. A method of treating a patient to resist cutaneous aging of the skin
caused by cross-linking of collagen in the skin due to ultraviolet
radiation, comprising applying to the skin an external preparation
comprising: at least 0.005 wt % of DL-.alpha.-tocopherol 2-L-ascorbic
phosphoric diester and/or a salt thereof; and at least 0.01 wt % of at
least one ultraviolet absorbing agent, whereby cross-linking of collagen
in the skin is suppressed when irradiated with ultraviolet rays, the wt %
is based on the weight of the entire composition.
2. The method of claim 1, wherein the amount of said DL-.alpha.-tocopherol
2-L-ascorbic phosphoric diester and/or a salt thereof is 0.005 to 0.2 wt
%.
3. The method of claim 1, wherein the amount of said ultraviolet absorbing
agent is 0.01 to 15.0 wt %.
4. The method of claim 2, wherein the amount of said ultraviolet absorbing
agent is 0.01 to 15.0 wt %.
5. The method of claim 1, wherein the ultraviolet absorbing agent is at
least one of benzophenone ultraviolet absorbing agent.
6. The method of claim 3, wherein the ultraviolet absorbing agent is at
least one of benzophenone ultraviolet absorbing agent.
7. The method of claim 4, wherein the ultraviolet absorbing agent is at
least one of benzophenone ultraviolet absorbing agent.
8. The method of claim 1, wherein the ultraviolet absorbing agent is
2-hydroxy-4-methoxybenzophenone or its salt.
9. The method of claim 2, wherein the ultraviolet absorbing agent is
2-hydroxy-4-methoxybenzophenone or its salt.
10. The method of claim 3, wherein the ultraviolet absorbing agent is
2-hydroxy-4-methoxybenzophenone or its salt.
11. The method of claim 4, wherein the ultraviolet absorbing agent is
2-hydroxy-4-methoxybenzophenone or its salt.
Description
FIELD OF THE INVENTION
The present invention relates to an external preparation and more
particularly, to an external preparation which is applied to the skin to
resist cutaneous aging.
BACKGROUND ART
The epidermis of the skin becomes thin with aging, and suffers from
symptoms such as the reduction in the production of keratin.
One of the important factors affecting cutaneous aging is age in a broad
view, but more direct causes are dryness, oxidization by active oxygen,
damage by ultraviolet rays (especially UV-A ultravioletrays which reaches
carium) and the like.
Various methods are conventionally taken in order to resist cutaneous
aging. For example, external preparations applied to the skin containing a
blend of various humectants for resisting cutaneous aging due to dryness,
those containing an antioxidant such as vitamin E for resisting cutaneous
aging due to oxidization, and those containing an absorbing agent for
resisting cutaneous aging due to ultraviolet rays are conventionally used.
Such conventional cutaneous aging resisting means are no better than a
symptomatic treatment, and cannot produce a sufficient cutaneous aging
resisting effect.
SUMMARY OF THE INVENTION
Accordingly, it is an object of the present invention to eliminate the
above described problems in the prior art and to provide an external
preparation which is capable of resisting cutaneous aging more
efficiently.
As a result of studies undertaken by the present inventors so as to achieve
this aim, it has been found that an excellent cutaneous aging resisting
effect is produced by combining a specific tocopherol derivative and an
ultraviolet absorbing agent. The present invention has been achieved on
the basis of this finding.
It is well known that the cross-linking of the collagen in the skin
increases with aging (Cutaneous Aging, edited by Albert M. Kligman and
Yoshio Takase, UNIVERSITY OF TOKYO PRESS, pp. 263 to 274, 1988 and
Sugiyama T., Fujimoto D., Arai C., and Hasegawa M., Biomed. Res. 8: pp.349
to 351, 1987).
It is also known that collagen is cross-linked by ultraviolet rays
(Fujimori E., FEBS Lett 235 (1 to 2) pp. 98 to 102, 1988).
Accordingly, the present inventors have aimed at production of an external
preparation which resists cutaneous aging by suppressing cross-linking of
the collagen in the skin.
In the first aspect of the present invention, an external preparation
comprises: at least about 0.005 wt % of DL-.alpha.-tocopherol 2-L-ascorbic
phosphoric diester and/or a salt thereof; and at least about 0.01 wt % of
at least one ultraviolet absorbing agent.
In the second aspect of the present invention, the amount of said
DL-.alpha.-tocopherol 2-L-ascorbic phosphoric diester and/or a salt
thereof is 0.005 to 0.2 wt %.
In the third aspect of the present invention, the amount of said
ultraviolet absorbing agent is 0.01 to 15.0 wt %.
In the fourth aspect of the present invention, an external preparation
comprises;
from about 0.005 to 0.2 wt % of DL-.alpha.-tocopherol 2- L-ascorbic
phosphoric diester and/or a salt thereof, and from about 0.01 to 15.0 wt %
of at least one ultrabiolet absorbing agent.
In the fifth aspect of the present invention, an external preparation
comprises: DL-.alpha.-tocopherol 2-L-ascorbic phosphoric diester and/or a
salt thereof, and at least one benzophenone ultraviolet absorbing agents.
In the sixth aspect of the present invention, an external preparation
comprises: from about 0.005 to 0.2 wt % of DL-.alpha.-tocopherol
2-L-ascorbic phosphoric diester and/or a salt thereof and from about 0.01
to 15.0 wt % of at least one benzophenone ultraviolet absorbing agent.
In the seventh aspect of the present invention, the ultraviolet absorbing
agent is 2- hydroxy-4-methoxybenzophenone or its salt.
In the eighth aspect of the present invention, a method of resisting
cutaneous aging comprises applying to the skin said external preparation
In the ninth aspect of the present invention, a preparation for resisting
cutaneous aging when applied to the skin comprises DL-.alpha.-tocopherol
2-L-ascorbic phosphoric diester and/or salt thereof, and at least one
benzophenone ultraviolet absorbing agents.
The structure of the present invention will be explained in detail
hereinunder.
The amount of DL-.alpha.-tocopherol 2-L-ascorbic phosphoric diester
(hereinunder referred to as "EPC") and/or a salt thereof in an external
preparation for application to the skin according to the present invention
is preferably 0.005 to 0.2 wt %.
An example of a preferred salt of EPC is alkali metal salts such as sodium
and potassium, and alkali earth metal salts such as calcium and magnesium
of EPC (hereinunder referred to as EPC-Na and the like).
If the amount of EPC is less than 0.005 wt %, it is sometimes impossible to
obtain a sufficient cutaneous aging resisting effect. Addition of more
than 0.2 wt % of EPC hardly increases the cutaneous aging resisting
effect.
In the present invention, at least one ultraviolet absorbing agent is used
in addition to EPC or a salt of EPC.
As the ultraviolet absorbing agent, ultraviolet absorbing agents which are
permitted as ingredients of ordinary cosmetics are used as occasion
demands. Examples thereof are:
cinamic acid ultraviolet absorbing agents such as 2-ethoxyethyl paramethoxy
cinnamate, isopropyl paramethoxy cinnamate, diisopropyl cinnamate,
ethylhexyl paramethoxy cinnamate, glyceryl diparamethoxy cinnamate
mono-2-ethyl hexanoate and octyl methoxy cinnamate;
benzoylmethane ultraviolet absorbing agents such as
butylmethoxybenzoylmethane and 4-tert-butyl-4'-methoxy-dibenzoylmethane;
bezophenone ultraviolet absorbing agents such as
glyceryl-mono-2-ethylhexanoyl-di-paramethoxybenzophenone,
2-2'-dihydroxy-4-methoxybenzophenone, 2-2'-dihydroxy-4,
4'-dimethoxybenzophenone, 2-hydroxy-4-methoxybenzophenone and sodium
2-hydroxy-4-methoxybenzophenone-5-sulfonate;
benzoic acid ultraviolet absorbing agents such as methyl
orthoaminobenzoate, 2-ethylhexyl-paradimethyl aminobenzoate and octyl
paradimethyl aminobenzoate;
benzoate ultraviolet absorbing agents such as glyceryl paraaminobenzoate,
amyl-para-dimethyl aminobenzoate and ethyl-4-bishydroxy propyl
aminobenzoate; and
other ultraviolet absorbing agents such as 2-ethylhexyl-2-cyano-3,
3'-diphenyl acrylate, digalloyl trioleate, 2-ethylhexyl salicylate,
homomethyl salicylate, guaiazulene and urocanic acid.
The amount of ultraviolet absorbing agent added is different depending upon
the type of ultraviolet absorbing agent, but it is generally 0.01 to 15.0
wt % of the total amount of external preparation.
If the amount of ultraviolet absorbing agent is less than 0.01 wt %, the
synergistic effect thereof and EPC is sometimes insufficient. Addition of
more than 15.0 wt % of ultraviolet absorbing agent hardly increases the
cutaneous aging resisting effect.
In addition to the above-described essential ingredients, it is possible to
add, if necessary, other ingredients which are used for ordinary cosmetics
and drugs or quasi-drugs for application to skin. Those ingredients are,
for example, vitamin A's such as vitamin A oil, retinol and retinol
acetate; vitamin B2's such as riboflavin, riboflavin butyrate and flavin
adenine dinulcleotide; vitamin B6's such as pyridoxine hydrochloride and
pyridoxine dioctanoate; vitamin C's such as L-ascorbic acid, dipalmitate
L-ascorbate, Na L-ascorbate-2-sulfate; pantothenic acids such as calcium
pantothenate, D-pantothenyl alcohol, pantothenyl ethyl ether and
acetylpantothenyl ethyl ether; vitamin D's such as ergocalciferol and
cholecalciferol; nicotinic acids such as nicotinic acid, nicotinic acid
amide, benzyl nicotinate; vitamin E's such as .alpha.-tocopherol,
tocopherol acetate, DL-.alpha.-tocopherol nicotinate and
DL-.alpha.-tocopherol succinate; other vitamins such as vitamin P and
biotin; amino acids and derivatives thereof such as glycine, alanine,
valine, leucine, isoleucine, serine, threonine, aspartic acid and salts
thereof, glutamic acid and salts thereof lysine, arginine, cysteine,
methionine, phenylalanine, tyrosine, histidine, tryptophane, proline,
N-acyl acidic amino acid salts such as diethyl-N-palmitoyl L asparaginate
and sodium N-coconut oil fatty acid-L-glutamate; acyl neutral amino acid
salts such as coconut oil fatty acid-sarcosine triethanol amine and
laurolylmethyl-.beta.-alanine sodium; pyrrolidonecarboxylic acid and salts
thereof, POE (40) hardened castor oil monopyrrogultamic monoisostearic
diester and coconut oil fatty acid-L-ethyl
arginate-DL-pyrrolidone-carboxylate; oil contents such as avocado oil,
palm oil, peanut oil, beef tallow, rice bran oil, jojoba oil, evening
primrose oil, carnauba wax, lanolin, liquid paraffin, squalane, isostearyl
palmitate, isostearyl alcohol and glycerin tri-2-ethylhexanate; humectants
such as glycerin, sorbitol, polyethylene glycol 1, 3-butylene glycol,
collagen, hyaluronic acid, chondroitin sulfuric acid and sodium dextran
sulfate; antioxidants such as sodium erisorbate and parahydroxyanisole;
surfactants such as sodium stearyl sulfate, cetyl sulfate diethanol amine,
cetyl trimethyl ammonium saccharin, polyethylene glycol isostearate,
glyceryl arachate, diglycerin diisostearate and phospholipid; antiseptic
agents such as ethyl para-hydroxybenzoate and butyl para-hydroxybenzoate;
antiphlogistic agents such as glycyrrhizic acid, glycyrrhetic acid,
salicylic acid derivative, hinokitiol, zinc oxide and allantoin; skin
beautifiers such as extract of placenta, glutathione and extract of
creeping saxifrage; various extracts such as extracts of phellodendron
bark, goldthread, peony, Japanese green gentian, birch, sage, loquat,
ginseng, aloe, mallow, iris, grape, coix seed, dishcloth gourd, lily,
saffron, Cnidium officinare Makino, giner, Saint-John's wort, rosemary and
garlic, vitalizers such as royal jelly, sensitizing dye, cholesterol
derivatives and extract of calf's blood; blood circulation facilitators
such as .gamma.-oryzanol; anti-srborrhoeic agents such as sulfur and
thianthol; thickening agents such as carboxyvinyl polymers, carboxymethyl
cellulose and carboxylhydroxypropyl cellulose; perfumes; water; alcohols;
coloring agents such as titanium yellow, carthamin and safflower red; and
resin powder such as polyethylene and nylon powders.
The external preparation according to the present invention may take any
given form. For example, it may be a soluble agent such as lotion, an
emulsified agent such as milky lotion and cream, an ointment, a dispersant
or an aerosol.
EMBODIMENTS
The present invention will be explained in detail with reference to
preferred embodiments. The present invention, however, is not restricted
to the embodiments.
Effect of ultraviolet rays in suppressing the cross-linking of collagen
A method of obtaining the ratio of cross-linking of collagen caused by
ultraviolet rays will first be explained.
Collagen was extracted from human placenta with pepsin and salted out for
purification (Nishihara T., and Miyata T., Collagen Symposium 3 pp. 66-93,
1962).
The purity of collagen measured 94% by electrophoresis (Hayashi T. and
Nagai Y., J. Biochem, 86 (2), pp. 453 to 459, 1979). The extracted and
purified collagen (final concentration; 1 mg/ml) was held in phosphate
buffered saline of pH 7.4 at 37.degree. C. to reconstruct collagen fiber,
and thereafter the collagen fiber was irradiated with ultraviolet rays
(TOSHIBA FL20S.BLB lamp, peak in the UV-A region: 365 nm) at an energy of
7.0 J/cm.sup.2. Each of the sample shown in Tables 1 and 2 was allowed to
coexist with collagen during irradiation.
Each sample was produced by mixing EPC-K and sodium
2-hydroxy-4-methoxybenzophenone-5-sulfonate as an ultraviolet absorbing
agent with phosphoric buffer as a base.
The ratio of cross-linking of the collagen irradiated with ultraviolet rays
was measured by electrophoresis and a densitometer (densitometer F-808 for
fluorescence, produced by COSMO corporation).
The suppression ratio of the cross-linking of collagen was obtained from
the following formula:
##EQU1##
(Reference: phosphate buffered saline)
The results of experiments are shown in the following.
TABLE 1
______________________________________
EPC Ultraviolet absorbing agent
Suppression ratio
______________________________________
0.5 5.0 80
0.3 5.0 77
0.2 5.0 82
0.1 5.0 85
0.05 5.0 84
0.01 5.0 79
0.005 5.0 72
0.001 5.0 61
0.0 5.0 56
______________________________________
As is obvious from Table 1, the preferred amount of EPC added is 0.05 to
0.2 wt %. When it was less than 0.005 wt %, an appropriate synergistic
effect was not obtained. On the other hand, even by adding more than 0.2
wt % of EPC, the increase in the effect was not observed.
TABLE 2
______________________________________
EPC Ultraviolet absorbing agent
Suppression ratio
______________________________________
0.1 20.0 80
0.1 15.0 85
0.1 10.0 79
0.1 5.0 85
0.1 1.0 83
0.1 0.5 72
0.1 0.1 81
0.1 0.05 77
0.1 0.01 71
0.1 0.005 61
0.1 0.0 57
0.0 0.0 56
______________________________________
As is obvious from Table 2, the preferred amount of ultraviolet absorbing
agent added is 0.01 to 15.0 wt %. When it was less than 0.01 wt %, an
appropriate synergistic effect was not obtained. On the other hand, even
by adding more than 15.0 wt % of EPC, the increase in the effect was not
observed.
As a result of these experiments, it was found that single use of either
EPC or an ultraviolet absorbing agent cannot efficiently suppress the
cross-linking of collagen.
A combination of another ascorbic acid or a derivative thereof did not
produce the excellent effect in suppressing the cross-linking of collagen
such as that described above.
TABLE 3
______________________________________
L-ascorbic acid
Ultraviolet absorbing agent
Suppression ratio
______________________________________
0.7 5.0 56
0.5 5.0 65
0.1 5.0 63
______________________________________
TABLE 4
______________________________________
Tocopherol Ultraviolet absorbing agent
Suppressing ratio
______________________________________
0.7 5.0 40
0.5 5.0 55
0.1 5.0 58
______________________________________
TABLE 5
______________________________________
Phosphate ascorbate
Ultraviolet absorbing agent
Suppression ratio
______________________________________
0.7 5.0 38
0.5 5.0 47
0.1 5.0 53
______________________________________
As is obvious from Tables 3 to 5, single use of either ascorbic acid or
tocopherol did not affect the suppression of the cross-linking of collagen
in the above-described manner. Even use of an ascorbic acid derivative
such as phosphate did not produce the synergistic effect, either.
In this way, it is observed that the action of suppressing the
cross-linking of collagen is furthered by the idiosyncratic synergistic
action of EPC and an ultraviolet absorbing agent.
The actual cutaneous aging resisting effect was examined by using hairless
mice.
9-year-week hairless mice were divided into three groups, each consisting
of three mice, and they were irradiated with ultraviolet rays from TOSHIBA
32BL lamp at a dosage of 14 J/cm2/day. 0.1 ml of a sample was applied to
each mouse immediately before irradiation. 10 days after irradiation, 3 g
of the skin was cut out and homogenized in 3% acetic acid. After
incubating the homogenized skin for one night, it was subjected to
centrifugal separation at a rate of 2000 rpm for 10 minutes. 5% trichloro
acetic acid was added to the precipitate to effect acid hydrolysis at
90.degree. C. for 30 minutes. After centrifugal separation at 2000 rpm for
10 minutes, the supernatant liquid was dialyzed and the hydroxyproline
content in the collagen was measured by a method of Stagemann and Stalder
(H. Stagemann and K stalder, Clinica Chemica Acta, 19, pp. 267 to 273,
1967) to calculate the amount of cross-linking collagen.
The composition of the sample liquid was as follows.
______________________________________
Basic preparation wt %
______________________________________
Citric acid 0.02
Sodium Citrate 0.08
Glycerin 5.0
Ethanol 5.0
Methyl para-hydroxybenzoate
0.1
Purified water balance
______________________________________
Group A (reference) . . . Basic preparation
Group B (Embodiment) . . . Basic preparation+EPC (0.2%)+sodium 2-hydroxy
4-methoxybenzophenone-5-sulfonate (1%)
Group C (Comparison) . . . Basic preparation+diisostearic acid L-ascorbin
(1%)+sodium 2-hydroxy 4-methoxybenzophenone-5-sulfonate(1%)
The suppression ratio of the cross-linking of collagen was calculated in
the above-described method
The results are shown in Table 6.
TABLE 6
______________________________________
Suppression ratio
______________________________________
Group A --
Group B 87
Group C 50
______________________________________
Concrete examples of the composition of the external preparation of the
present invention will now be shown. The amount of ingredient is shown by
wt %. Each of external preparations produced the synergistic effect and
the cutaneous aging resisting effect.
EXAMPLE 1
Lotion
______________________________________
(1) EPC 0.05
(2) Sodium 2-hydroxy 4-methoxybenzophenone-5-sulfonate
0.1
(3) Tocopherol acetate 0.01
(4) Glycerin 4.0
(5) 1,3-butylene glycol 4.0
(6) Ethanol 8.0
(7) Polyoxyethylene (60) hardened castor oil
0.5
(8) Methyl para-hydroxybenzoate
0.2
(9) Citric acid 0.05
(10) Sodium citrate 0.1
(11) Perfume 0.05
(12) Purified water balance
______________________________________
<Process>
EPC, sodium 2-hydroxy-4-methoxybenzophenone-5-sulfonate, citric acid,
sodium citrate, glycerin and 1,3-butylene glycol were dissolved in
purified water. Separately from this, polyoxyethylene (60) hardened castor
oil, tocopherol acetate, perfume and methyl para-hydroxybenzoate were
dissolved in ethanol. The latter solution was added to the purified water
solution for solubilization, and the resultant solution was filtered to
obtain lotion.
<Result>
______________________________________
Sample Suppressing Ratio
______________________________________
Example 1 78
Without UV absorbent (component (2))
47
Without EPC (component (1))
39
Without UV absorbent and EPC
38
(components (1) and (2))
______________________________________
EXAMPLE 2
Cream
______________________________________
(1) Cetostearyl alcohol 3.5
(2) Squalane 40.0
(3) Bee wax 3.0
(4) Reduced lanolin 5.0
(5) Ethyl para-hydroxybenzoate
0.3
(6) Polyoxyethene (20) sorbitan mono palmitate
2.0
(7) Monoglyceride stearate
2.0
(8) Sodium N-stearoyl glutamate
0.5
(9) 2-hydroxy-4-methoxy-benzophenone
0.5
(10) Octyl methoxycinnamate
1.0
(11) Retinol acetate 2.0
(12) Evening primrose oil
0.05
(13) Perfume 0.03
(14) EPC-Na 0.1
(15) 1,3-butylene glycol 5.0
(16) Polyethylene glycol 1500
5.0
(17) Purified water balance
______________________________________
<Process>
Cetosteatyl alcohol, squalane, bee wax, reduced lanolin, ethyl
para-hydroxybenzoate, polyoxyethylene (20) sorbitan monopalmitate,
monoglyceride stearate, sodium N-stearoyl glutamate,
2-hydroxy-4-methoxy-benzophenone, octyl methoxycinnamate, retinol acetate
and evening primrose oil were dissolved under heating (oil parts).
Separately from this, EPC-Na, 1,3-butylene glycol and polyethylene glycol
1500 were dissolved in purified water and heated to 75.degree. C. (water
parts). Oil parts were added to water parts under stirring. After
pulverizing the emulsified particles by a homomixer, the mixture was
rapidly cooled under stirring to produce cream
<Result>
______________________________________
Sample Suppressing Ratio
______________________________________
Example 2 82
Without UV absorbent (components (9), (10))
38
Without EPC--Na (component (14))
36
Without UV absorbents and EPC--Na
36
(components (9), (10) and (14))
______________________________________
EXAMPLE 3
Milky lotion
______________________________________
(1) EPC--Mg 0.2
(2) 2-ethylhexyl para-dimethylaminobenzoate
0.1
(3) Mono-2-ethylhexyl diparamethoxycinnamate
0.2
(4) Stearic acid 1.5
(5) Cetyl alcohol 0.5
(6) Bee wax 2.0
(7) Polyoxyethylene (10) monooleate
2.0
(8) L-arginine 0.3
(9) Na L-glutamate 0.02
(10) PCA--Na 0.05
(11) Na hyaluronate 0.01
(12) Propylene glycol 5.0
(13) Glycerin 3.0
(14) Ethanol 3.0
(15) Ethyl para-hydroxybenzoate
0.3
(16) Perfume 0.03
(17) Carboxyvinyl polymer
0.12
(18) Purified water balance
______________________________________
<Process>
Perfume was dissolved in ethanol (alcohol parts). EPC-Mg, L-arginine, Na
L-glutamate, PCA-Na, Na hyaluronate, propylene glycol, glycerin and
carboxyvinyl polymer were dissolved in purified water under heating and
the mixture was held at 70.degree. C. (water parts). The other ingredients
were mixed and dissolved under heating, and the mixture was held at
70.degree. C. (oil parts). The oil parts were added to the water parts for
preliminary emulsification and the mixture was uniformly emulsified by a
homomixer. The alcohol parts were added to the emulsion under stirring.
The mixture was cooled to 30.degree. C. under stirring to obtain milky
lotion.
<Result>
______________________________________
Sample Suppressing Ratio
______________________________________
Example 3 82
Without UV absorbents (components (2), (3))
45
Without EPC--Mg (component (1))
42
Without UV absorbents and EPC--Mg
40
(components (1), (2) and (3))
______________________________________
EXAMPLE 4
Foam mask
______________________________________
(1) EPC--K 0.02
(2) 4-tert-butyl-4'-methoxy-dibenzoylmethane
0.5
(3) Stearic acid 1.0
(4) Behenylic acid 1.0
(5) Self-emulsification type glycerin monostearate
1.5
(6) Polyoxyethylene monostearate
2.5
(7) Batyl alcohol 1.5
(8) Perfume 0.05
(9) Glycerin 5.0
(10) 1,3-butylene glycol 5.0
(11) Polyethylene glycol 1500
3.0
(12) Methyl para-hydroxybenzoate
0.1
(13) Potassium hydroxide 0.15
(14) Purified water balance
(15) Liquified petroleum gas
6.0
(16) Dimethyl ether 2.0
______________________________________
<Process>
EPC-K, glycerin, 1,3-butylene glycol, polyethylene glycol 1500, methyl
para-hydroxybenzoate and potassium hydroxide were added to purified water
and dissolved under heating at 70.degree. C. The other ingredients except
under heating, added to the mixture and were uniformly mixed. The
resultant mixture was charged in a container. Finally, liquefied petroleum
gas and dimethyl ether were added to the mixture as a spraying agent,
thereby producing a foam mask.
<Result
______________________________________
Sample Suppressing Ratio
______________________________________
Example 4 77
Without UV absorbent (components (2))
41
Without EPC--K (component (1))
43
Without UV absorbent and EPC--K
39
(components (1) and (2)
______________________________________
EXAMPLE 5
Ointment
______________________________________
(1) EPC--Ca 0.1
(2) Octyl paradimethyl aminobenzoate
4.0
(3) Butylmethoxybenzoylmethane
4.0
(4) Tocopherol acetate
0.5
(5) Retinol palmitate
1.0
(6) Stearyl alcohol 18.0
(7) Japan wax 20.0
(8) Polyoxyethylene (10) monooleate
0.25
(9) Glycerin monostearate
0.3
(10) Vaseline 32.0
(11) Purified water balance
______________________________________
<Process>
EPC-Ca was added to purified water and the mixture was held at 70.degree.
C. (water parts). The other ingredients were mixed and dissolved at
70.degree. C. (oil parts). The oil parts were added to the water parts and
the mixture was uniformly emulsified by a homomixer. The mixture was then
cooled to obtain ointment.
As described above, according to the external preparation of the present
invention, since DL-.alpha.-tocopherol 2-L-ascorbic phosphoric diester
and/or a salt thereof and at least one ultraviolet absorbing agent are
contained, it is possible to suppress the cross-linking of collagen and to
produce an excellent cutaneous aging resisting effect.
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